2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. HDAC-IN-53

HDAC-IN-53 是一种具有口服活性的，选择性 HDAC1-3 抑制剂，IC50 值分别为 47 nM、125 nM 和 450 nM。HDAC-IN-53 不抑制 II 类 HDAC (HDAC4、5、6、7、9; IC50>10 μM)。HDAC-IN-53 诱导 caspase 依赖性细胞凋亡。HDAC-IN-53 可显着抑制裸鼠中人肿瘤异种移植物的生长和携带 MC38 结肠癌的免疫活性小鼠的肿瘤生长。

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HDAC-IN-53 Chemical Structure

HDAC-IN-53 Chemical Structure

CAS No. : 2921948-27-6

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HDAC-IN-53 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer[1].

IC50 & Target[1]

HDAC1

47 nM (IC50)

HDAC2

125 nM (IC50)

HDAC3

450 nM (IC50)

HDAC4

>10 μM (IC50)

HDAC5

>10 μM (IC50)

HDAC6

>10 μM (IC50)

HDAC7

>10 μM (IC50)

HDAC8

>10 μM (IC50)

HDAC9

>10 μM (IC50)

体外研究
(In Vitro)

HDAC-IN-53 (化合物 19h) 对一组癌细胞系具有良好的抗增殖活性，例如 MC38 (IC50=0.66 μM)、HCT116 细胞 (IC50=0.56 μM)[1]。
HDAC-IN-53 (0.1-1 μM; 24 小时) 在 MC38 细胞中引起 G0/G1 细胞周期停滞，在 HCT116 细胞中诱导 G2/M 细胞周期停滞[1]。
HDAC-IN-53 (0.1-1 μM; 24 小时) 以剂量依赖的方式上调 cleaved caspase-3 和 cleaved PARP 的表达[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC-IN-53 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MC38 and HCT116 cells
Concentration: 0.1, 0.3, 1 μM
Incubation Time: 24 h
Result: Caused G0/G1 cell cycle arrest in MC38 cells and induced G2/M cell cycle arrest in HCT116 cells.
Significantly decreased the proportion of S phase cells in MC38 cells.

Western Blot Analysis[1]

Cell Line: MC38 and HCT116 cells
Concentration: 0.1, 0.3, 1 μM
Incubation Time: 24 h
Result: Upregulated the expressions of cleaved caspase-3 and cleaved PARP in a dose-dependent manner.
体内研究
(In Vivo)

HDAC-IN-53 (60 或 120 mg/kg; 灌胃给药; 每日一次; 持续 15 天) 通过直接肿瘤生长抑制和间接免疫细胞介导的抗肿瘤作用发挥抗肿瘤活性[1]。
Pharmacokinetic Parameters of HDAC-IN-53 in Mice[1].

IV (5 mg/kg) PO (20 mg/kg)
Tmax (h) 0.42
Cmax (ng/mL) 8129 9558
AUC0-t (ng/mL∗h) 5864 15278
t1/2 (h) 0.85 2.49
F (%) 65.1%

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 Mice or athymic nude mice (female, 6-8 weeks old) with MC38 cells[1]
Dosage: 60 or 120 mg/kg
Administration: PO; daily for 15 days
Result: Yielded TGI values of 60.3 and 87.6%, respectively.
Increased the percentage of CD4+ T cells.
分子量

461.90

Formula

C23H20ClN7O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HDAC-IN-53 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC-IN-532921948-27-6HDACApoptosisHistone deacetylasesOrallyclass II HDACcaspase-dependentMC38colon cancerHCT116PARPcaspase-3Inhibitorinhibitorinhibit

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